Biopharmaceutics classification and absorption mechanisms primary study on four kinds of flavonoids

• Published in: Zhongguo zhongyao zazhi Vol. 41; no. 7; p. 1198
• Main Authors: Li, Hui-Fang, Zhang, Dong, Qu, Wen-Jun, Wang, Hai-Lin, Liu, Yang, Borjigdai, Almaz, Cui, Jian, Dong, Zheng-Qi
• Format: Journal Article
• Language: Chinese
• Published: China 01.04.2016
• Subjects: Biopharmaceutics - classification; Caco-2 Cells; Drugs, Chinese Herbal - pharmacokinetics; Flavonoids - pharmacokinetics; Humans; Intestinal Absorption; Permeability; Solubility; biopharmaceutics classification system (BCS); solubility; absorption mechanism; flavonoids; permeability
• ISSN: 1001-5302
• DOI: 10.4268/cjcmm20160707

The solubility and permeability on four kinds of flavonoids (kaempferol, hesperidin, apigenin, genistein) were test according to the theory of biopharmaceutics classification system (BCS), and their absorption mechanism. The solubility was investigated by the method in determination of solubility of "Chinese Pharmacopoeia 2010". To detect appearance permeability of compounds mentioned above, the appropriate concentrations were selected by the MTT method in cell transfer experiments in Caco-2 cell model, which established by in vitro cell culture method. Therefore, these compounds were classified with BCS according to solubility and permeability. In addition, to explore absorption mechanisms, the experiments in three different concentrations of compounds in high, medium and low in bidirectional transformation methods in Caco-2 cell model contacted. The study indicated that all of kaempferol, hesperidin, apigenin, genistein have the characteristics in low solubility and high permeability, which belong to BCSⅡ, and the absorption mechanism of kaempferol was active transportation. Whereas, hesperidin, apigenin, genistein were passive transportation. In this study, it carried out initial explorations on establishment of determination for solubility and permeability in flavonoids, and provided theoretical reference for further research on BCS in traditional Chinese medicine.